JAK2-IN-7

Name: JAK2-IN-7
Brand: MedChemExpress
SKU: HY-131906
Rating: 4.5 (1 reviews)

Cat. No.: HY-131906 Purity: 99.15%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

JAK2-IN-7 is a selective JAK2 inhibitor with IC₅₀s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3^V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.

For research use only. We do not sell to patients.

JAK2-IN-7 Chemical Structure

CAS No. : 2593402-36-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 455	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 455	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2550	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

JAK1

42 nM (IC₅₀)

JAK2

3 nM (IC₅₀)

JAK3

94 nM (IC₅₀)

Tyk2

75 nM (IC₅₀)

FLT3

62 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
L02	IC₅₀	7.22 μM Compound: 13ac	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33256400]
Vero	IC₅₀	6.75 μM Compound: 13ac	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33256400]

In Vitro

JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2^V617F cells^[1].
JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase^[1].
JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	SET-2 cells
Concentration:	10-160 nM
Incubation Time:	24 hours
Result:	Induced cell arrest in the G0/G1 phase in a concentration-dependent manner.

Apoptosis Analysis^[1]

Cell Line:	SET-2 cells
Concentration:	0.05-1.6 μM
Incubation Time:	2 hours
Result:	Induced apoptosis in SET-2 cells.

In Vivo

JAK2-IN-7 (15-60 mg/kg; p.o.; daily for 16 days) shows potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model^[1].
JAK2-IN-7 (30-60 mg/kg; p.o.; q.d. for 16 day) significantly ameliorates the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SET-2 cell-inoculated xenograft NOD/SCID mouse model^[1]
Dosage:	15, 30, and 60 mg/kg
Administration:	Orally daily for 16 days
Result:	Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.

Molecular Weight

459.59

Formula

C₂₆H₃₃N₇O

CAS No.

2593402-36-7

Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=C(N=C(N=C1)NC2=CC=C3CN(CCC3=C2)C(/C=C/CN(C)C)=O)C4=CN(N=C4)C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (543.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1759 mL	10.8793 mL	21.7585 mL
5 mM	0.4352 mL	2.1759 mL	4.3517 mL
10 mM	0.2176 mL	1.0879 mL	2.1759 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.15%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (244 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Yang T, et al. N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms [published online ahead of print, 2020 Nov 30]. J Med Chem. 2020;10.1021/acs.jmedchem.0c01488. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1759 mL	10.8793 mL	21.7585 mL	54.3963 mL
	5 mM	0.4352 mL	2.1759 mL	4.3517 mL	10.8793 mL
	10 mM	0.2176 mL	1.0879 mL	2.1759 mL	5.4396 mL
	15 mM	0.1451 mL	0.7253 mL	1.4506 mL	3.6264 mL
	20 mM	0.1088 mL	0.5440 mL	1.0879 mL	2.7198 mL
	25 mM	0.0870 mL	0.4352 mL	0.8703 mL	2.1759 mL
	30 mM	0.0725 mL	0.3626 mL	0.7253 mL	1.8132 mL
	40 mM	0.0544 mL	0.2720 mL	0.5440 mL	1.3599 mL
	50 mM	0.0435 mL	0.2176 mL	0.4352 mL	1.0879 mL
	60 mM	0.0363 mL	0.1813 mL	0.3626 mL	0.9066 mL
	80 mM	0.0272 mL	0.1360 mL	0.2720 mL	0.6800 mL
	100 mM	0.0218 mL	0.1088 mL	0.2176 mL	0.5440 mL

JAK2-IN-7 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JAK2-IN-72593402-36-7JAKFLT3ApoptosisJanus kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3V617FmutationphosphorylationantitumorSET-2xenograftmodelInhibitorinhibitorinhibit

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Complete Stock Solution Preparation Table

JAK2-IN-7 Related Classifications

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